Depression Of Activity Research Articles

Potential of Nerium oleander as a traditional medicine: A review of phytoconstituents and CNS-depressant properties

Since ancient times, people have used medicinal plants to treat various diseases. Nerium oleander is a toxic plant due to the presence of various cardiac glycosides. Oleander, at a dose of 50 mg kg-1 inhibits Na+/K+ ATPase pump in mice. Despite being toxic, it is used in traditional medicine. Almost all of the parts of oleander plant contain various phytochemicals such as phenols, tannins, flavonoids, coumarins, sterols, triterpenes, alkaloids, and different types of cardenolides. Oleander extract has neuroprotective, sedative, and anticonvulsant properties, especially against ischemic stroke. Cardenolides like nerizoside, neritaloside, odoroside-H, and neridiginoside offer advantages when used as CNS depressants. CNS depressant action of oleander is primarily due to a rise in GABA levels. At low to moderate dose, it shows depressant activity but in high doses, body became motionless inducing tremors and lethargy. Oleanderʼs dual role of toxic and therapeutic activity raises concerns about its application. Yet due to presence of vast constituents, it can be used for modern medicine.

Role of Ayurveda medicine in the management of Amashaya Arbhuda w.s.r. to Carcinoma of Stomach

Due to faulty lifestyle, altered food habits and chronic psychological stress and mental depression, the incidence of Malignancy has been raised. Carcinoma of stomach is one such disorder which is commonly seen in Indian population. Symptoms like pain abdomen, burning sensation of the stomach, malena, weight loss, loss of appetite and anaemia are the common clinical features of this disease. Ayurveda medicine is beneficial in the cases with early diagnosis. After radical excision of the active lesion, palliative treatment can be given by using Ayurveda medicine. In Ayurveda, Vyadhi Pratyanika Aushadhi Prayoga, Yogasana and Pranayama, Assurance, changes in food and life style and Pathapathya Prayoga are advised. Medicines having actions like Anticancer, cytotoxic, Shoolahara, Antacid, antispasmodics, antidepressant, anxiolytic, antistress, adaptogenic, CNS depressant, Balya, Brimhala, Ojaskara, immunomodulator and cytoprotective actions are used as palliative measures. In this paper, the role of Ayurveda medicines in the management of Amashaya Arbhuda w.s.r. to carcinoma of stomach is discussed elaborately.

CNS DEPRESSANT ACTIVITY OF KASHAYA OF ASOKA – SARACA ASOCA ROXB. DE (WILDE.)

Ayurveda explains chikitsa (treatment – mode to attain health) as a conglomeration of chatushpada’s (four limbs). Pharmacological categorization of drugs can be explored for the first time from the Charaka Samhita, Shadvirechana Shatasriteeya Adhyaya. Asoka - Saraca asoca [Roxb] de Wilde has been included in the Vedanasthapana mahakashaya (group of drugs which alleviates a specific sensation) mentioned by Acharya Charaka, which is explained as streenam uchrokanashanaya by the Nighantukaara’s. The etymology of soka is chittavikalatha, which is a ‘lead’ to the action of a drug on “manasika bhava’s”. In clinical experience, apart from the pain, associated symptoms like nausea, vomiting, delirium, insomnia, emotional instability, nervousness, irritability, anger, and fear are also relieved by its usage. Till now, the pharmacological action of Asoka on “manasika bhava’s” remains unexplored. Hence, a preliminary experimental study has been undertaken on the reverse pharmacological aspect to assess the action of this drug on CNS. The depressant action of drugs on CNS is mediated through both neural and hormonal mechanisms. The immediate reduction in spontaneous motor activity was achieved through the neural mechanism, and the prolonged effect was achieved through the hormonal action. The drug possesses bitter principles. The functional bitter taste is expressed in brain cells by bitter taste receptors T2R’s. T2R-4, T2R-107, and T2R-38 transcripts are found in the brain stem, cerebral cortex and cerebellum. The drug is a potent source of phytoestrogen, which has oestrogen-mimicking action. The drug significantly reduces spontaneous motor activity in the CNS depressant activity study on all assessment days, with a p-value.

Da-Chuan-Xiong Decoction Ameliorates Sodium Sensitivity and Plasma Norepinephrine via Attenuation of Brain Oxidative Stress in the DOCA-Salt Hypertensive Rats.

Da-Chuan-Xiong Decoction (DCXD) is an aqueous extract from a classic Chinese herbal formula composed of dried rhizomes of Ligusticum chuanxiong Hort and Gastrodia elata Bl. in the mass ratio of 4 : 1. It has been long used to treat chronic cardiovascular disease caused by blood stasis and wind pathogen in the clinic. This experimental study aimed to investigate the blood pressure (BP)-lowering effect of DCXD treatment on hypertension and underlying mechanisms. Male Sprague-Dawley rats were used in the experiment, and the hypertensive models were created by administering deoxycorticosterone acetate (DOCA) in conjunction with a high salt intake in uninephrectomized rats. DCXD was administered to hypertensive rats by oral gavage daily at a dose of 5 g/kg or 2.5 g/kg bodyweight for 28 days. The brain sodium sensitivity, ENaC function, superoxide anion level, NADPH oxidase activity, and expression of ENaC, p67phox, p47phox, and Rac1 in the paraventricular nucleus were assessed by using the appropriate methods. The 28 days of DCXD (5 g/kg) treatment significantly reduced the increased BP effectively, inhibited the enhanced heart index, kidney index, and 24 h urinary protein, and improved the progressive pathological changes of heart and kidney, which was comparable to that of the positive control amlodipine. DCXD treatment also caused a marked reduction in plasma norepinephrine and induced a significant improvement in brain sodium sensitivity and ENaC function in DOCA-salt hypertensive rats. Rats in DCXD-treated groups also exhibited decreased superoxide anion levels and NADPH oxidase activity in the paraventricular nucleus. The level of ENaC, p67phox, and Rac1 protein expression in the paraventricular nucleus was significantly downregulated by DCXD treatment in DOCA-salt hypertensive rats. These findings indicate that the depressor action and sympathetic inhibition of DCXD on salt-sensitive hypertension may be by ameliorating brain sodium sensitivity, modulating ENaC function, and inhibiting the expression of ENaC and NADPH oxidase in the hypothalamic paraventricular nucleus.

The mechanism of 25-hydroxycholesterol-mediated suppression of atrial β1-adrenergic responses.

25-Hydroxycholesterol (25HC) is a biologically active oxysterol, whose production greatly increases during inflammation by macrophages and dendritic cells. The inflammatory reactions are frequently accompanied by changes in heart regulation, such as blunting of the cardiac β-adrenergic receptor (AR) signaling. Here, the mechanism of 25HC-dependent modulation of responses to β-AR activation was studied in the atria of mice. 25HC at the submicromolar levels decreased the β-AR-mediated positive inotropic effect and enhancement of the Ca2+ transient amplitude, without changing NO production. Positive inotropic responses to β1-AR (but not β2-AR) activation were markedly attenuated by 25HC. The depressant action of 25HC on the β1-AR-mediated responses was prevented by selective β3-AR antagonists as well as inhibitors of Gi protein, Gβγ, G protein-coupled receptor kinase 2/3, or β-arrestin. Simultaneously, blockers of protein kinase D and C as well as a phosphodiesterase inhibitor did not preclude the negative action of 25HC on the inotropic response to β-AR activation. Thus, 25HC can suppress the β1-AR-dependent effects via engaging β3-AR, Gi protein, Gβγ, G protein-coupled receptor kinase, and β-arrestin. This 25HC-dependent mechanism can contribute to the inflammatory-related alterations in the atrial β-adrenergic signaling.

Impact of COVID-19 Vaccine Rollout on Mental Health, Social Determinants of Health, and Attitudes Among Individuals With COPD.

Social distancing early in the COVID-19 pandemic helped mitigate viral spread and protect vulnerable populations. Broad availability of vaccines allowed social re-integration, but effects on mental health, social determinants of health, and attitudes among individuals with COPD, who are high-risk for adverse outcomes following COVID-19 infection, are unknown. Participants in the Losartan Effects on Emphysema Progression (LEEP) trial were recruited into an ancillary study from May-November 2020. Study coordinators administered telephone questionnaires to evaluate respiratory symptoms (COPD Assessment Test [CAT]), anxiety (Generalized Anxiety Disorder-7 [GAD-7]) and depressive (Patient Health Questionnaire [PHQ-8]) symptoms, social isolation, instrumental support, and attitudes and actions related to the COVID-19 pandemic. Generalized estimating equation models evaluated changes in patient-reported scores from the period before vaccine availability (pre-vaccine, May-December 2020) to the post-vaccine period (May 2021-September 2022). Of 157 enrolled participants, 138 were interviewed during both periods. Compared with the pre-vaccine period, severe respiratory symptoms (CAT>20) were higher in the post-vaccine period (odds ratio [OR] 1.36, 95% confidence interval [95%CI]: 1.00-1.85), as were moderate anxiety symptoms (GAD-7≥10; OR 1.65, 95%CI: 1.11-2.46) and moderate depressive symptoms (PHQ-8≥10; OR 1.77, 95%CI: 1.22-2.55). Social isolation improved, though not significantly, and instrumental support was unchanged. In the post-vaccine period compliance with COVID-19 mitigation strategies remained high and governmental healthcare entities were viewed as trustworthy by fewer respondents. Despite a trend towards less social isolation following broad availability of COVID-19 vaccines, individuals with COPD reported worse symptoms, and greater anxiety and depressive symptoms compared to the pre-vaccine period.

Adiponectin affects ileal contractility of mouse preparations.

Adiponectin (ADPN) has been reported to induce inhibitory effects on gastric motor activity, which, being a source of peripheral satiety signals, would contribute to the central anorexigenic effects of the hormone in rodents. However, peripheral satiety signals can also originate from the small intestine. Since there are no data on the effects of ADPN in this gut region, the present study aimed to investigate whether ADPN affects murine ileal contractility. Immunofluorescence experiments and Western blot were also performed to reveal the expression of ADPN receptors. Mechanical responses of ileal preparations were recorded in vitro via force-displacement transducers. Preparations showed a tetrodotoxin- and atropine-insensitive spontaneous contractile activity. Electrical field stimulation (EFS) induced tetrodotoxin- and atropine-sensitive contractile responses. ADPN induced a decay of the basal tension and decreased the amplitude of either the spontaneous contractility or the EFS-induced excitatory responses. All ADPN effects were abolished by the nitric oxide (NO) synthesis inhibitor NG-nitro l-arginine. The expression of the ADPN receptor, AdipoR1, but not AdipoR2, was also revealed in enteric glial cells. The present results offer the first evidence that ADPN acts on ileal preparations. The hormone exerts inhibitory effects, likely involving AdipoR1 on enteric glial cells and NO. From a physiological point of view, it could be hypothesized that the depressant action of ADPN on ileal contractility represents an additional peripheral satiety signal which, as also described for the ileal brake, could contribute to the central anorexigenic effects of the hormone.NEW & NOTEWORTHY This study provides the first evidence that adiponectin (ADPN) is able to act on ileal preparations. Functional results demonstrate that the hormone, other than causing a slight decay of the basal tension, depresses the amplitude of both spontaneous contractility and neurally induced excitatory responses of the mouse ileum through the involvement of nitric oxide. The expression of the ADPN receptor AdipoR1 and its localization on glial cells was revealed by Western blot and immunofluorescence analysis.

Modulating Hyperpolarization-Activated Cation Currents through Small Molecule Perturbations: Magnitude and Gating Control.

The hyperpolarization-activated cation current (Ih) exhibits a slowly activating time course of the current (Ih) when the cell membrane is hyperpolarized for an extended duration. It is involved in generating electrical activity in various excitable cells. Numerous structurally distinct compounds or herbal drugs have the potential to impact both the magnitude and gating kinetics of this current. Brivaracetam, a chemical analog of levetiracetam known to be a ligand for synaptic vesicle protein 2A, could directly suppress the Ih magnitude. Carisbamate, an anticonvulsant agent, not only inhibited the Ih amplitude but also reduced the strength of voltage-dependent hysteresis (Hys(V)) associated with Ih. Cilobradine, similar to ivabradine, inhibited the amplitude of Ih; however, it also suppressed the amplitude of delayed-rectifier K+ currents. Dexmedetomidine, an agonist of α2-adrenergic receptor, exerted a depressant action on Ih in a concentration-dependent fashion. Suppression of Ih amplitude was observed when GAL-021, a breathing control modulator, was present at a concentration exceeding 30 μM. Lutein, one of the few xanthophyll carotenoids, was able to suppress the Ih amplitude as well as to depress Hys(V)'s strength of Ih. Pirfenidone, a pyridine derivative known to be an anti-fibrotic agent, depressed the Ih magnitude in a concentration- and voltage-dependent fashion. Tramadol, a synthetic centrally active analgesic, was shown to reduce the Ih magnitude, independent of its interaction with opioid receptors. Various herbal drugs, including ent-kaurane-type diterpenoids from Croton tonkinensis, Ganoderma triterpenoids, honokiol, and pterostilbene, demonstrated efficacy in reducing the magnitude of Ih. Conversely, oxaliplatin, a platinum-based chemotherapeutic compound, was observed to effectively increase the Ih amplitude. Collectively, the regulatory effects of these compounds or herbal drugs on cellular function can be partly attributed to their perturbations on Ih.

Neuropharmacological study of Moringa olifera

Objective: Moringa olifera is a medicinal plant widely used in many parts of the world for hypertension, pain and epilepsy. The aim of this study was to determine the effect of M. olifera aqueous leaf, root and steam extract on neurobehavioral activities of healthy mice. Method: Male mice were randomly divided into a control group (given 0.9% NaCl orally) and three groups treated with the extract at doses of 100, 200, and 400 mg/kg/day for 14 consecutive days. Neuropharmacological activity were evaluated by neuro-muscular coordination (rota rod treadmill), pain (hot plate and acetic acid-induced abdominal constriction). Administration of M. olifera extract had a significant and dose dependent antinociceptive action in both thermal and chemical tests (p < 0.05). The extract (400 mg/kg) caused a reduction in exploration activity and neuromuscular coordination, and decreased the mobility time in the FST, suggesting an antidepressant-like action. Motor activity was not significantly affected by any of the doses used. Conclusion: The results suggest that the plant aqueous extract may have a dose-dependent central nervous system (CNS) depressant action.

A Phyto Pharmacological Comparitive Review on Curcuma Species

Since the dawn of time, medicinal plants have been employed by local populations as a source of healing throughout the healthcare system to demonstrate their efficacy. Some of the results have sparked the development of plant-based medications. The most intricate of interactions would be the investigation of how plants work. This essay examines the function of contemporary pharmacology in relation to a variety of plant derived medicines that has been used for millennia and were know to ancient civilizations. The skill of pharmacists and doctors to engage to the challenges that have arose with the propagation of professional services in the assistance of mans life has increased as a result of wisdom of the development of ideas related to the use of herbal medicines as well as the evolution of awareness. It has been noticed that the plant contained antibacterial, antioxidant, analgesic antifungal, antiasthmatic ,smooth pain reliever, locomotor depressant, anti convulsant and muscle relaxing actions as well as anti inflammatory characteristics. It is now thought of as a useful source of distinctive natural compounds for the creation of medicines against different diseases. According to phytochemical studies, the main chemical components of Curcuma aromatica and Curcuma caesia are terpenoids, flavonoids, phenolic compounds, tannins, inorganic compounds, organic acids and anthocyanin.

EVALUATION OF CNS DEPRESSANT AND BEHAVIORAL ACTIVITY OF AN ETHANOL EXTRACT OF ZIZIPHUS JUJUBA (BER) IN MOUSE MODEL

Objective: Ziziphus jujuba, known as Ber (Hindi), is an indigenous herb found in India. Z. jujuba has been used to treat various diseases such as respiratory system diseases (asthma, cough, and laryngitis), gastrointestinal problems (constipation, colitis, and liver diseases), as well as cardiovascular and genitourinary system diseases. Seeds and fruit have been also reported to have central nervous system (CNS) depressant effect. Hence, in this study, neuropharmacological effects of leaves are studied which are not reported previously. Z. jujuba extract’s potential to depress the CNS and affect behavior was examined in this study, along with the phytochemicals that may be responsible for these effects. Methods: 400 mg/kg of the extract was administered intraperitoneally. As a benchmark, diazepam (2 mg/kg body weight i.p.) was used. ANOVA and Dunnett’s tests were used to evaluate the data. The results were all presented as Mean (SEM) values. p>0.05 was regarded as meaningful. Result: The outcome of the study demonstrated that ethanol extract of Z. jujuba (400 mg/kg i.p.) reduced locomotion, caused muscle relaxation, and had anti-anxiety effects. Conclusions: Ethanols extract of Z. jujuba leaves exhibits CNS depressant action and significant anxiolytic activity comparable to diazepam.

Inhibition of mitochondrial respiration by general anesthetic drugs

General anesthetic drugs have been associated with various unwanted effects including an interference with mitochondrial function. We had previously observed increases of lactate formation in the mouse brain during anesthesia with volatile anesthetic agents. In the present work, we used mitochondria that were freshly isolated from mouse brain to test mitochondrial respiration and ATP synthesis in the presence of six common anesthetic drugs. The volatile anesthetics isoflurane, halothane, and (to a lesser extent) sevoflurane caused an inhibition of complex I of the electron transport chain in a dose-dependent manner. Significant effects were seen at concentrations that are reached under clinical conditions (< 0.5 mM). Pentobarbital and propofol also inhibited complex I but at concentrations that were two-fold higher than clinical EC50 values. Only propofol caused an inhibition of complex II. Complex IV respiration was not affected by either agent. Ketamine did not affect mitochondrial respiration. Similarly, all anesthetic agents except ketamine suppressed ATP production at high concentrations. Only halothane increased cytochrome c release indicating damage of the mitochondrial membrane. In summary, volatile general anesthetic agents as well as pentobarbital and propofol dose-dependently inhibit mitochondrial respiration. This action may contribute to depressive actions of the drugs in the brain.

The ventilatory depressant actions but not the antinociceptive effects of morphine are blunted in rats receiving intravenous infusion of L-cysteine ethyl ester

This study demonstrates that intravenous infusion of the cell-penetrant thiol ester, L-cysteine ethyl ester (L-CYSee), to adult male Sprague-Dawley rats elicited (a) minor alterations in frequency of breathing, expiratory time, tidal volume, minute ventilation, or expiratory drive but pronounced changes in inspiratory time, end-inspiratory and expiratory pauses, peak inspiratory and expiratory flows, EF50, relaxation time, apneic pause, inspiratory drive and non-eupneic breathing index, (b) minimal changes in arterial blood-gas (ABG) chemistry (pH, pCO2, pO2, SO2) and Alveolar-arterial (A-a) gradient (index of alveolar gas exchange), and (c) minimal changes in antinociception (tail-flick latency). Subsequent injection of morphine (10 mg/kg, IV) elicited markedly smaller effects on the above parameters, ABG chemistry, and A-a gradient in rats receiving L-CYSee, whereas morphine antinociception was not impaired. Infusions of L-cysteine or L-serine ethyl ester (oxygen rather than sulfur moiety), did not affect morphine actions on ABG chemistry or A-a gradient. L-CYSee (250 μmol/kg, IV) injection elicited dramatic changes in ventilatory parameters given 15 min after injection of morphine in rats receiving L-CYSee. Our findings suggest that (a) L-CYSee acts in neurons that drive ventilation, (b) L-CYSee reversal of the adverse actions of morphine on ventilation, ABG chemistry and A-a gradient may be via modulation of intracellular signaling pathways activated by morphine rather than by direct antagonism of opioid receptors since morphine antinociception was not diminished by L-CYSee, and (c) the thiol moiety of L-CYSee is vital to efficacy, (d) intracellular conversion of L-CYSee to an S-nitrosylated form may be part of its mechanism of action.

KATP channels as ROS-dependent modulator of neurotransmitter release at the neuromuscular junctions

AimsNeurotransmitter release requires high energy demands, making the nerve terminals metabolically fragile and susceptible to oxidative stress. ATP-sensitive potassium (KATP) channels can be an important regulator orchestrating the influence of metabolic-related signals on exocytosis. Here, the relevance of ROS in KATP channel-dependent control of neurotransmitter release at the frog neuromuscular junction was studied. MethodsMicroelectrode recordings of end plate potentials at the distal and proximal compartments of nerve terminals as well as fluorescent techniques were used. Key findingsActivation of KATP channels in the proximal region suppressed evoked and spontaneous release in a lipid raft-dependent manner. Activation of KATP channels in the distal region reduced solely evoked release which was preserved after lipid raft disruption. Chelation of ROS potentiated the effects of KATP channel activation and unmasked the effects of KATP channel blocker on evoked exocytosis. Activation or inhibition of KATP channels suppressed or enhanced the depressant action of extracellular adenosine on evoked exocytosis. This was accompanied with an increase or decrease in adenosine-induced ROS production, respectively. KATP channel-dependent modulation of adenosine action was halted by antioxidant and NADPH-oxidase inhibitor. Also, activation of KATP channels led to an increase in ROS production suppressing the negative effects of extracellular ATP on evoked release in a ROS-dependent manner. SignificanceKATP channel-mediated modulation of release has specific features in distal and proximal compartments and depends on endogenous ROS levels and lipid raft integrity. Activation of KATP channels suppresses the action of extracellular adenosine and ATP on evoked release by increasing ROS production.

Beneficiation of Nickel from Ultramafic Ores: Using Sodium Citrate as a Green Processing Reagent

The processing of ultramafic ores requires fine grinding, which can result in slime-coating of the nickel-bearing mineral, pentlandite, by the phyllosilicate gangue mineral, serpentine. This lowers nickel recovery and concentrate grade during froth flotation operations. The presence of divalent cations in process water exacerbates the detrimental effects of phyllosilicates on nickel recovery by enhancing the positive surface charge of serpentine and causing charge reversal of pentlandite. To mitigate these issues, an environmentally benign, nontoxic, and biodegradable reagent, sodium citrate, was used in this study to chelate divalent cations on the pentlandite surface and desorb them from the mineral surface. The metal-citrate complexes adsorb onto the positively charged serpentine surface, reversing its charge. Sodium citrate was able to restore the surface charge and hydrophobicity of pentlandite, reverse the charge of serpentine, desorb the divalent cations from the mineral surface, and prevent MgO gangue recovery to the froth phase. Microflotation studies demonstrated that upon the addition of sodium citrate, nickel recovery increased from 74 to 96% and nickel grade was improved from 11 to 15.1% . The hydrophobicity of pentlandite was restored upon conditioning with citrate as evident by increase in water static contact angle from 50° to 70° , DLVO interactions showed that addition of citrate prevents slime coating of pentlandite by serpentine. The results demonstrated the depressive and dispersive action of sodium citrate.

Examination of the periaqueductal gray as a site for controlling arterial pressure in the conscious spontaneously hypertensive rat.

Our understanding of central nervous system regulation of the set-point of arterial pressure remains incomplete, especially in conditions of hypertension. The ventrolateral periaqueductal gray (vlPAG) is of particular interest given that its acute activation induces hypotension and sympatho-inhibition in anaesthetised, normotensive animals, and recent preliminary studies have shown that vlPAG stimulation can reduce blood pressure in refractory hypertensive patients. To assist our mechanistic understanding, we investigated whether electrical stimulation of the vlPAG had depressor actions in a model of neurogenic hypertension, the spontaneously hypertensive (SH) rat. We found that electrical stimulation of the lateral and vlPAG (2-6V, 20-40Hz, 0.18-0.2ms pulse width) decreased arterial pressure (-19±4mmHg, n=8) and heart rate (median-18bpm) in anaesthetised SH rats. In contrast, in conscious freely-moving SH rats fitted with blood pressure telemetry, stimulation of this same region produced failed to evoked a hypotensive response (n=13; either no change, n=9; or an increase in arterial pressure of 23±4mmHg, n=4). The hypotensive action of the vlPAG observed in anaesthetised animals has been attributed to inhibition of pre-sympathetic neurones originating in the rostral ventrolateral medulla. We therefore used an un-anaesthetised, decerebrate SH rat preparation to investigate whether activation of vlPAG neurons produced sympatho-inhibition that might be below the threshold at which a peripheral vascular response could be observed. Only sympatho-excitatory responses to electrical and excitatory amino acid microinjections were observed, and these were evoked from both the dorsal and ventral PAG; no responses were evoked from the vlPAG. We conclude that the vlPAG is not a reliable antihypertensive locus in the awake SH rat. We discuss the potential importance of the state-dependency of the hypotensive response that can be evoked from the vlPAG, which has important implications for translating to humans.

Central Nervous System Activity of 1-aryl-2(thiomethylene benzimidazol-2-yl)-4-(phenyl/p-chlorophenyl)-imidazoles and 1-aryl-2-sulphono-[benzimidazol-2-yl]-methyl-4-(phenyl/p-chlorophenyl)-imidazoles

1-Aryl-2-mercapto-4-(phenyl/p-chlorophenyl)-imidazoles (Ia-1) were condensed with 2-chloromethyl benzimidazole (II) in presence of sodium hydroxide in ethanol to get 1-aryl-2-thiomethylene benzimidazol-2-yl-4-(phenyl/p-chlorophenyl)-imidazoles (IIIa-1). These compounds (IIIa-1) were subsequently oxidised by hydrogen peroxide to get 1-aryl-2-sulphono-[benzimidazol-2-yl]-methyl-4 and (phenyl/p-chlorophenyl)-imidazoles (Iva-1). All the compounds (IIIa-1) and (Iva-1) exhibited central nervous system depressant action on albino mice. All the compounds are non-toxic and possess some sedative activity.

Микроэлектрофизиологическое изучение соотношения возбудительных и тормозных синаптических процессов в кортиконигральной проекции к SNс на модели болезни Паркинсона

In series experiments on 9 Albino rats (250 g) the comparative analyses of single neuron’s impulse activity of Substantia nigra compacta – SNc at high frequency stimulation (HFS) of the brain primary motor cortex (M1) in norm (107 neurons, n=4) and on the model of Parkison’s disease (PD) (105 neurons, n=5) has been conducted. Analyses of relative degree of depressor and excitatory effects frequency intensity on the base of spikes average frequency diagrams, represented as a disc diagram (in %) resulted in the following conclusions. In SNc neurons on the model of PD the poststimulus manifestations of depressor activity completely absent, but tetanic potentiation in both sequences 1,65- and 2,02-multiple exceeded of those in the norm. The comparative analyses of pre- and poststimulus frequency activity of SNc neurons on the model of PD, led to the conclusion that it is considerably higher in comparison with the norm. It has been revealed vulnerability of depressor poststimulus effects of SNc neurons, even their full absence, that in its turn, testifies about more involvement of SNc in PD.

Pharmacoepidemiology of yellow trumpet flower

Because synthetic pharmaceuticals may produce various side effects and unfavorable consequences, the use of natural plants in therapy is currently more common than synthetic goods. Tecoma stans is a plant found in most tropical countries. This plant belongs to the Bignoniaceae family and is already used in ancient medicine in various countries such as India and Pakistan. This plant has a large number of active chemical ingredients and has pharmacological effects. Many researchers have explored pharmacological screening, and ongoing research is being conducted in that plant. The goal of this study was to update the plant's research collections for pharmacological screening. The review focuses on several researches, such as pharmacognostical studies and in-vitro and in-vivo screening of numorous Tecoma stans components. The various parts of the plants were concluded to have various pharmacological actions such as anti-inflammatory, analgesic, anticancer cardioprotective effect, genotoxic, cytotoxicity, wound healing, antihyperglycemic, protect CNS, gastric ulcer healing, antiproliferative, antioxidant, anti-microbial, haemolytic activity, anti-lipoxygenase, and acetyl-cholinesterase inhibitory activities. This review was then used to guide future study on this plant. A member of the trumpet vine family, Tecoma stans, has been documented for a variety of pharmacological properties. The current research focuses on the neuropharmacological activities of several Tecoma stans extracts. The CNS depressive action was addressed first, followed by the analgesic activity, and then the impact of various extracts on Albino mice was examined.

Behavioural Effects of Aerial Parts of Alysicarpus glumaceus Vahl DC in Murine Models

AbstractBackground Alysicarpus glumaceus has been reported to be used in managing patients with neuropsychiatric disorders. This work aimed to determine the behavioural effects of aerial parts of Alysicarpus glumaceus in murine models.MethodThe behavioural effects of the drug extract was evaluated using elevated zero maze (EZM), stair case test (SCT) and the open field test (OFT) while beam walking was used to test for motor coordination deficit and stimulant activity in mice at doses of 500, 1000 and 1500 mg/kg using diazepam (0.05 mg/kg) as the standard and normal saline (NS) as the control.ResultsAll the test doses of the extract reduced the stretch attend posture and head dips as well as the number of rearing without significant decrease in the number of stairs climbed in the EZM and SCT respectively when compared to NS. In the OFT, Alysicarpus glumaceus extract increased the number of square crossing but it was insignificant (p&gt;0.05). The extract at 1000 and 1500 mg/kg significantly (p&lt;0.01) decreased the number of rearing; while at 500 mg/kg it significantly (p&lt;0.001) decreased the number of rearing. At all the test doses used, there was no significant difference in time to reach the goal box and number of foot slips, however, mice given 500 mg/kg of the extract produced a significant (p&lt;0.05) increase in time spent on the beam.ConclusionThe findings revealed that the aerial parts of Alysicarpus glumaceus possesses central nervous system depressant actions.